An inhibitor of JAK1, JAK2, JAK3, and TYK2
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Delgocitinib

Item No. 38307

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3S,4R)-3-methyl-β-oxo-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octane-1-propanenitrile
CAS Number
1263774-59-9
Synonyms
  • JTE-052
Molecular Formula
C16H18N6O
Formula Weight
310.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/ml
λmax
214, 285 nm
SMILES
O=C(N(C1)[C@]2([C@H]1C)CN(C3=C(C=CN4)C4=NC=N3)CC2)CC#N
InChi Code
InChI=1S/C16H18N6O/c1-11-8-22(13(23)2-5-17)16(11)4-7-21(9-16)15-12-3-6-18-14(12)19-10-20-15/h3,6,10-11H,2,4,7-9H2,1H3,(H,18,19,20)/t11-,16-/m0/s1
InChi Key
LOWWYYZBZNSPDT-ZBEGNZNMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $85

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    5 mg

    $380

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    10 mg

    $590

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    25 mg

    $1,053

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    Product Description

    Delgocitinib is an inhibitor of JAK1, JAK2, JAK3, and tyrosine kinase 2 (TYK2; IC50s = 2.8, 2.6, 13, and 58 nM, respectively).1 It is selective for JAK1, JAK2, JAK3, and TYK2 over lymphocyte cell-specific tyrosine kinase (LCK; IC50 = 5,800 nM). Delgocitinib inhibits IL-31-induced increases in STAT3 phosphorylation levels in A549 cells (IC50 = 25 nM). It reduces IL-31-induced scratching in mice in a dose-dependent manner.2 Formulations containing delgocitinib have been used in the treatment of atopic dermatitis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Noji, S., Hara, Y., Miura, T., et al. Discovery of a Janus kinase inhibitor bearing a highly three-dimensional spiro scaffold: JTE-052 (delgocitinib) as a new dermatological agent to treat inflammatory skin disorders. J. Med. Chem. 63(13), 7163-7185 (2020).

    2. Yamamoto, Y., Otsuka, A., Nakashima, C., et al. Janus kinase inhibitor delgocitinib suppresses pruritus and nerve elongation in an atopic dermatitis murine model. J. Dermatol. Sci. 97(2), 161-164 (2020).